The drug cyclodol is a drug from a psychiatric clinic

Pharmacodynamics and pharmacokinetics

Cyclodol is a centrally acting anticholinergic drug that disrupts the connections between dopamine and acetylcholine in the central nervous system. This reduces the cholinergic effects caused by dopamine deficiency.

Like other anticholinergic drugs, therapy reduces tremor and has an antispasmodic effect; to a lesser extent, there is an effect on muscle rigidity and bradykinesia.

Pharmacokinetic information

After oral administration, trihexyphenidyl is rapidly absorbed and penetrates the blood-brain barrier. The half-life ranges from 6-10 hours. There are no data regarding distribution, binding to plasma proteins in the blood, metabolism and clearance.

The drug cyclodol is a drug from a psychiatric clinic

articles » Types of drugs » The drug cyclodol - a drug from a psychiatric clinic
Cyclodol belongs to the group of hallucinogenic drugs or psychedelics. This drug is the oldest of all drugs that are used to treat Parkinson's disease.

It began to be used as a psychedelic drug in the Soviet Union in the late 50s and early 60s, and in terms of popularity and consequences of use it became a Soviet analogue of phencyclidine.

Cyclodol is a drug from a psychiatric clinic. Aminazine appeared in medicine these years, which revolutionized previously used methods and approaches to mental illness.

Aminazine was widely used in those days - it was prescribed to almost all patients who suffered from various forms of schizophrenia. But it also had side effects - impaired coordination of movements, it is also called neuroleptic syndrome.

Therefore, in order to prevent complications, almost all patients were prescribed the drug cyclodol along with aminazine.

Patients soon realized that a small excess of the dose of cyclodol causes a state of intoxication, and an even larger overdose when withdrawing aminazine leads to various kinds of hallucinations.

The drug cyclodol and other drugs can currently be purchased on the streets along with narcotic substances. The main place of distribution of the drug cyclodol is schools.

According to the stories of drug addicts, many drug dealers offer even younger schoolchildren to try pills, which do no harm and are used as medicines.

According to statistics, for 24% of patients suffering from heroin addiction, the first experience of drug use was associated with taking the drug cyclodol at school or at a disco.

Drug cyclodol: application and phases

The first phase is associated with increased mood, euphoria.

The initial stage develops 20-30 minutes after taking the tablets. First, a feeling of warmth appears, especially in the arms and legs. A person feels a pleasant lightness in the body.

Sounds become distinct, colors become colorful and bright. Everyday worries and problems cease to worry and fade into the background.

The narcoman becomes talkative, movements that were initially smooth begin to speed up.

Everything that happens around can cause laughter. This state of mild excitement lasts about 20 minutes and then the second phase begins.

The second phase begins after 40-45 minutes and has a different effect - inhibited movement, the desire to sit down or lie down, decreased activity, dizziness and a feeling of weightlessness and “wool” in the legs.

The addict may feel either hot or cold. A person seems to see himself from the outside; his consciousness can be separated from the body. At the same time, the entire surrounding environment changes before his eyes - objects become fuzzy, unsteady, fluid, moving. Different patients perceive reality in different ways: these sensations can be pleasant, or they can be frightening. In this state, the addict is unable to formulate thoughts correctly or is simply unable to communicate.

In this phase, the addict loses the sense of his own “I”, loses control over his own thoughts, the addict’s personality becomes completely weak-willed and suggestible.

According to the testimony of one patient in a rehabilitation center, the girl was raped by 11 young men at a time when she was in a state of drug intoxication with the drug cyclodol.

The characteristic difference between cyclodol and other hallucinogens, the picture of drug intoxication is very well remembered. An episode in the girl’s life involving rape ruined her psyche for the rest of her life.

The second phase lasts from 2 to 4 hours, depending on the amount of the drug taken.

The third phase begins with the appearance of hallucinations, but this phase is not obligatory, that is, it cannot occur in all cases. The presence of this phase depends on the individual characteristics of the human body and on the dosage of the drug Cyclodol.

While in this phase, a person ceases to orient himself in space and time. At first, he experiences various forms of deception of perception - strange sounds, rustling, clicking, ringing, stomping, grinding and others. Then hallucinations may suddenly appear in the image of various people or animals. Images can move, talk and order a person to do something, instill an idea and set a goal.

According to the story of one of the patients, a “strange grandfather without eyes” appeared in front of him, who ordered him to lie under the train. It happened outside the city, at the dacha. The patient lay down on the rails at one of the railway stations. By a happy coincidence, there was a break in the train schedule and the man remained alive.

The patient said that he understood that this did not exist in reality, that it was just a hallucination, but he was unable to resist - it was easier to obey than to fight this image. The experience of hallucinations can last from 2 to 4 hours, also depending on the dose.

The fourth phase is the final stage of drug intoxication with cyclodol.

The body becomes heavy, the former lightness disappears. The person experiences terrible fatigue, complete exhaustion and inability to do anything.

Severe drowsiness sets in, the addict really wants to sleep, but most of them cannot sleep.

This condition can last for a very long time; it usually normalizes 8-12 hours after the third phase.

Signs of cyclodol use

A person who uses the drug cyclodol has a number of characteristic external signs: pale face, noticeable blush, reddened lips.

People from the outside may get the impression that it is made up with decorative cosmetics.

Among the external signs, mild twitching of the facial muscles and tremors of the limbs are also often noted. Also noticeable are the convulsive movements of the mouth and fingers.

Narcologists conducted studies that showed that out of 82 patients under the age of 18, 66 people experienced discomfort when using cyclodol for the first time.

Most often they talk about horror and nightmare. Even the feeling of lightness during the second phase seemed ominous and frightening to them.

But what is surprising is that despite all these “horrors” and “nightmares”, 90% of those examined continue to use this drug cyclodol.

Cyclodol: dependence and withdrawal syndrome

If a drug addict suddenly stops taking this medication after regular use of cyclodol, which lasted several months, then he experiences persistent discomfort and the need to take the drug.

Mental dependence develops 2-5 months after regular use of cyclodol. The need to use the drug again increases gradually.

The interval between doses varies from 24 to 36 hours. If a person tries to stop using it, then he feels a decrease in muscle tone, general physical weakness, irritability, stress and anger at the world around him appear. Thoughts about cyclodolus crowd out all life guidelines, values ​​and hobbies. An addict can give up studying and work, leave home, and not care about loved ones.

When about a year passes after the start of cyclodol use, the picture of life becomes even more depressing. Small muscle cramps become frequent, for example, endless, continuous clenching and unclenching of the fingers into a fist.

A person becomes restless, he cannot sit in one place for a long time, cannot maintain balance, and constantly makes many useless and involuntary movements.

With cyclodol withdrawal syndrome (withdrawal syndrome), all these disorders intensify even more. These signs also include weakness, chills, excessive sweating, nausea, vomiting, diarrhea, muscle and joint pain.

If a person’s nervous system weakens and tremors increase, then these symptoms can develop into real epileptic seizures.

A common occurrence of withdrawal syndrome is toxic psychosis or cyclodolium fever.

Such psychosis is dangerous because the addict does not feel the line between hallucinations and attacks of the fever itself. Psychosis can be mistaken for pleasure, a person may not even feel the difference.

One of the patients at the rehabilitation center spoke about the state of psychosis when using cyclodol:

“I lay in the room and had a heart-to-heart talk with a huge and kind dog. I liked the dog and it was pleasant to talk to her, although I was a little afraid of her. But suddenly there was some kind of thunder or blow outside the window, similar to a thunderclap, and a crowd of aggressive and angry men with sticks in their hands appeared in the room. They started beating the dog with sticks and accusing me of letting her out of some cage with my father, and the dog itself was extremely dangerous. I experienced wild fear and climbed out the window (fortunately, the teenager lived on the second floor). I don’t remember anything else. I don’t know what happened next. I know that my father found me some time later under the window with my teeth knocked out, with bruises and signs of beatings, and I had a stick clutched in my hand. My father said that I didn’t understand or understand anything at all, I just repeated that I had to kill someone and muttered some incomprehensible words under my breath. He tried to take the stick away from me, but he couldn’t do anything. Then I ended up in the hospital on a drip, because he couldn’t get me out of this state on his own...”

It is necessary to note that the body cannot tolerate a large number of such conditions. During the fourth or fifth such fever, young people risk dying from cardiac arrest and cerebral edema.

Cyclodol addiction rapidly leads to disruption of the normal functioning of the brain and nerve cells.

After 6 months of taking cyclodol, a person’s memory is impaired, often people are not even able to remember a phone number or address, in some cases the memory may be short-term.

Due to long-term use of the drug cyclodol, a person loses the ability to think logically and rationally. Self-esteem not only decreases, it begins to be absent, since the addict is no longer able to see himself from the outside. Such signs can lead to dementia and complete loss of personality.

Indications for use of Cyclodol

The main indications for the use of Cyclodol are parkinsonism ( and Little's disease ) of any etiology and neuroleptic extrapyramidal disorders .

In addition, the drug is used as monotherapy or in combination with Levodopa for the treatment of spastic paralysis caused by damage to the extrapyramidal system.

In some cases, it helps to reduce tone and improve movements with paresis .

“Question to the expert”: V.B. Dutov’s answers to questions about the Use of long-acting antipsychotics in the practice of outpatient psychiatric services

December 18, 2021, 11:50 Ivan Martynikhin

Dear colleagues,
In the ROP pro-Schizophrenia a section “ Question to an Expert ” has been opened, where everyone has the opportunity to directly ask questions regarding assistance to people with schizophrenia, leading domestic scientists and health care organizers. Today we are publishing answers to questions regarding the Use of long-acting injection antipsychotics in the practice of outpatient psychiatric services

Invited expert: Vladimir Borisovich Dutov – Candidate of Medical Sciences, chief physician of the St. Petersburg State Budgetary Institution “Psychoneurological Dispensary No. 1” (St. Petersburg), Associate Professor of the Department of Psychiatry and Narcology of Northwestern State Medical University named after I.I. Mechnikov. The institution headed by Vladimir Borisovich has accumulated extensive experience in the differentiated use of long-acting antipsychotics, both traditional and atypical.

Answers on questions

Question 1

Dear Vladimir Borisovich, based on your practice and the practice of your doctors, do you think that managing a patient on monotherapy with a long-acting antipsychotic helps to keep the patient in remission? And if not, what can you add? — Goremyko A.V., Moscow, PB No. 1

Answer:

Dear colleague! According to the literature, and in particular, according to the results of the PROSIPAL study, which involved 715 people, including 180 patients from many cities in Russia, it was shown that 85% of patients on Xeplion monotherapy did not have new exacerbations of schizophrenia for two years. Modern long-acting antipsychotic drugs suggest their use in the form of monotherapy, since they have a sufficient antipsychotic effect. Monotherapy is the most acceptable method, both from the point of view of the patient and from the point of view of the doctor, since the patient does not have the opinion that he is receiving a “hodgepodge of drugs”, and the doctor has a clear understanding of the essence of the treatment process, while compliance and confidence increase that the patient is actually receiving treatment.

In case of insufficient dosage of a long-acting antipsychotic, exacerbations are likely, and in this case it is possible to add tablet forms of the drug already used for a short time to therapy. For example, according to the experience of our doctors, with a standard dosage of Xeplion 75 mg once every 4 weeks, in case of exacerbation of existing chronic symptoms or the emergence of new phenomena, it is advisable to prescribe Invega followed by a transition to a higher dosage of Xeplion the next month. The combination of long-acting antipsychotic drugs with other drugs, such as oral antipsychotic drugs, is potentially possible, but is undesirable, since their combined use can lead to a significant increase in the risk of side effects, and data on the safety of their simultaneous use are limited.

In a situation where the proper antipsychotic effect from a long-acting antipsychotic drug is not observed, first of all, it is necessary to analyze whether the dosage of the drug prescribed to the patient is sufficient and, if necessary, increase the dosage of the drug on the day of the scheduled injection (up to this point it is permissible to increase the dosage of the drug by prescribing the same drug per os).

Thus, in our practice, we try to avoid simultaneous prescribing of two antipsychotic drugs to a patient, but combination with other groups is possible - tranquilizers, antidepressants, mood stabilizers. We believe that managing the patient on monotherapy with long-acting antipsychotics is sufficient to keep him in remission.

Question 2

What is the fate of piportil and imap? — Abdulkadyrov Abdulkadyr Omarovich, Khasavyurt, clinic

Answer:

Dear colleague! Today, piportil and imap are discontinued. Previously, these drugs were used mainly for inpatient treatment. At the same time, IMAP had a rather labor-intensive prescription regimen, and piportil had to be administered only in a glass syringe. Currently, they are almost completely ousted from the market by more modern antipsychotic drugs and we do not use them in our practice.

Question 3

Dear Vladimir Borisovich, please tell me, if my patient with schizophrenia receives several antipsychotics, how can he switch to injectable paliperidone in this case? Should we cancel everything and focus only on it or gradual cancellation? — Mikhail, St. Petersburg

Answer

Dear colleague! In this case, of course, it matters which antipsychotics we are talking about. In general, the instructions for using Xeplion detail the procedure for transferring from various antipsychotics. Thus, when switching from risperidone, the dose of the drug may be gradually reduced over one week due to the risk of withdrawal symptoms, such as insomnia. Our clinical experience and literature data have shown that the doses of olanzapine and quetiapine should be continuously reduced over 3-4 weeks, due to the risk of withdrawal symptoms accompanied by blocking of cholinergic, histaminergic and alpha-1-adrenergic receptors. When switching from aripiprazole and amisulpride, the first initiating injection of Xeplion is given the day after taking the last tablet. When transferring from Invega, standard initiation of Xeplion therapy is acceptable. The first injection of Xeplion is made the next day after taking the last Invega tablet. When transferring from Rispolept-Consta, usually immediately maintain a maintenance dose of Xeplion in a therapeutic dose corresponding to the previous dosage of Rispolept-Consta.

In any case, it is advisable to follow the instructions for use of medications. For patients who have never previously taken oral paliperidone, oral or injectable risperidone, tolerability with oral paliperidone or oral risperidone should be assessed before initiating treatment with Xeplion. At the beginning of treatment with Xeplion, previously used oral antipsychotic drugs, as mentioned above, can be gradually withdrawn, while the risk of developing so-called “rebound” psychoses must be taken into account, which necessitates the need to carefully monitor the patient’s current mental state. In our practice, transferring patients to injectable paliperidone therapy with gradual withdrawal of previous therapy takes on average about two weeks.

Question 4

Dear Vladimir Borisovich! My question is more about traditional long-acting antipsychotics. Using these drugs in your institution, are you trying to switch the patient from taking oral forms or are you more likely to use injections as an addition to therapy with tablet drugs? — Kuznetsov Sergey Alexandrovich, Rep. Komi, Komi Republican Psychiatric Hospital

Answer

Dear colleague! Oral forms are used in patients determined to take daily oral therapy. The dosage form of Xeplion, which allows it to be used once a month, unlike oral antipsychotics, provides confidence in patient compliance. This result is achieved due to regular visits to the doctor, improved adherence, a decent quality of life for the patient and due to the convenience of therapy, a decrease in the number of relapses and readmissions. In the vast majority of cases, monotherapy with an antipsychotic drug is the preferred choice in therapy and allows minimizing the possible risks of adverse events and treatment complications.

To date, combination therapy with antipsychotic drugs does not show a significant increase in effectiveness, but reliably leads to an increase in the number of complications from therapy. At our institution, we strive to follow current thinking and evidence-based approaches in the treatment of patients and avoid the combination of long-acting and oral antipsychotics in most cases. However, depending on the dynamics of the clinical picture, in some cases we add therapy with antidepressants or anxiolytics.

It is important to note that we make maximum use of atypical prolongations to form better and longer remissions in patients with dangerous tendencies, patients from the ADN and APLiN list. In this group of patients, the use of long-acting antipsychotics is a priority, which once again emphasizes the enormous importance of these drugs for outpatient practice.

Question 5

Dear Vladimir Borisovich, I heard that in St. Petersburg there is a practice of prescribing Xeplion in an acute condition in order to subsequently treat the patient on monotherapy. Tell me, is this true and how to act in this case from a practical point of view? What is the algorithm? — Andrey Feklistov, Moscow

Answer

Dear colleague! According to the instructions for medical use of the drug Xeplion, its use in acute psychomotor agitation or in a severe psychotic state, when immediate control of symptoms is necessary, is not recommended by the manufacturer and, obviously, the drug cannot be used in inpatient or, especially, outpatient practice. This is due to the fact that Xeplion, after injection into the deltoid muscle, reaches its peak therapeutic concentration only after 14 days, and into the gluteal muscle only after 13-17 days. Accordingly, it will not be possible to achieve a quick and complete effect to relieve acute symptoms. Moreover, the introduction of Xeplion without a sensitivity test is inappropriate. In such cases, it is possible to “cover” in the first stages of treatment with standard injectable neuroleptics and benzodiazepines. It is optimal to initiate Xeplion therapy at the stage of inpatient treatment with adjustment of therapy and reaching a mental state when further treatment with the drug can be continued in the form of monotherapy in selected dosages. Thus, the active use of atypical prolongs to an even greater extent implies interconnection and continuity in the work of inpatient and outpatient care. If it is necessary to treat long-acting injectable drugs in patients with mild to moderate psychotic states who have previously responded to therapy with oral forms of paliperidone or risperidone, Xeplion can be used without prior stabilization with oral drugs of this group, which can be successfully implemented in outpatient clinics. Our institution has such experience with the use of Xeplion in the intensive care unit for psychiatric care.

Question 6

Dear Vladimir Borisovich, how many patients are on long-acting antipsychotics? And is it only patients with schizophrenia? — Andrey Feklistov, Moscow

Answer

Dear colleague! If by long-acting antipsychotics you mean drugs such as Rispolept-Consta, Xeplion, Trevicta, then we are trying to provide these drugs to the maximum number of patients who meet the selection criteria. These are young age, social safety, ability to work, first psychotic episode and others. We can say with absolute certainty that the ability to prescribe long-acting atypical antipsychotic drugs is a revolutionary acquisition, primarily for outpatient psychiatric care. This is the most preferred and increasingly relevant type of drug therapy for patients. Moreover, recently we have been making our choice in favor of modern atypical long-acting antipsychotic drugs, as they are better tolerated, effective, safe and form the necessary compliance in partnerships with patients, creating the basis for overcoming stigmatization. The instructions state the indications as: treatment of schizophrenia and prevention of relapse of schizophrenia in adult patients. Treatment of schizoaffective disorders as monotherapy or as part of combination therapy with mood stabilizers and antidepressants in adult patients.

Indeed, these drugs are now widely used to treat schizophrenia and schizoaffective psychosis. We believe that one of the most effective areas for the use of atypical prolongs should be the early treatment of initial schizophrenic symptoms within the framework of the first episode clinic, when the use of such an expensive but highly effective drug is most economically justified. There are recommendations for their use in the case of affective psychoses, but in these situations the issue is resolved individually. In our institution, prolongs are actively used in the intensive psychiatric care unit, day hospital and rehabilitation department. In addition, some patients suffering from schizophrenia, schizoaffective and schizoform disorders receive extended periods of treatment in local psychiatric care as part of free additional drug provision. In this case, the number of patients receiving long-acting antipsychotics as part of additional drug provision is determined by the availability of drugs in pharmacies.

Question 7

How do primary patients without an official diagnosis of schizophrenia (for example, with F23) receive expensive extensions from you?

Answer

Dear colleague! In St. Petersburg, for a long time, there has been a register of patients provided with medicines at the expense of the constituent entities of the Federation. The inclusion of patients in the register is determined by regulations and includes a wide range of mental disorders from F20 to F29. The availability of the drug in pharmacies that provide preferential additional drug coverage, in turn, depends on the amount of funding. Although prescribing atypical long-acting antipsychotics specifically to patients diagnosed with “acute and transient mental disorder” (F 23) may not be very appropriate, because mental disorders of this spectrum require recovery within 2-3 months.

In addition, in St. Petersburg, in accordance with the Order of the Health Committee, the work of interdistrict medical commissions has been organized, which coordinate the prescription of expensive drugs, including Xeplion and Trevicta, based on the submitted medical documentation, the clinical picture and the presence of appropriate criteria for prescribing the drug.

Question 8

How to transfer a patient from Clopixol Depot to Xeplion? Because Xeplion has an activating effect, whether Klopixol tablets should be left together with Xeplion or canceled at the same time.

Answer

Dear colleague! As stated in the instructions, for patients who have never previously taken oral paliperidone and oral or injectable risperidone, a tolerability study with oral paliperidone or oral risperidone should be conducted before starting treatment with Xeplion. At the beginning of treatment with Xeplion, previously used orally administered antipsychotic drugs can be gradually withdrawn, while, as already mentioned, it is necessary to take into account the risk of developing so-called “rebound” psychoses, which necessitates the need to carefully monitor the patient’s current mental state.

If the patient receives long-acting injectable antipsychotics, treatment with Xeplion begins immediately with a maintenance dose at the time of the next scheduled injection. Treatment with Xeplion should be continued once a month.

Other features of the transition and administration of Xeplion for various patient transfer schemes should be carefully read in the instructions for the medical use of Xeplion. So, when transferring from clopixol depot to xeplion, as well as from other typical depot antipsychotics (haloperidol decanoate, fluphenazine decanoate, and flupenthixol decanoate), we try to use xeplion on the date of the planned depot injection in a maintenance dosage without the initiation of therapy stage. At the same time, we prefer to conduct a tolerability test a few days before the intended injection (when clopixol is still working) (for example, with the drug Invega). A tolerability test is necessary if the patient has not previously taken oral paliperidone or oral or injectable risperidone. If necessary, the patient continues to receive clopixol tablets for some time with a gradual reduction in dosage and subsequent discontinuation.

Question 9

To whom do you prescribe Xeplion, and to whom do you prescribe Rispolept consta? How do you divide such patients? By symptoms? This is also an atypical prolongation.

Answer

Dear colleague! If we compare Xeplion and Rispolept-Consta, the antipsychotic effect of both drugs is approximately the same (high affinity for serotonin 5-HT2 receptors and dopamine D2 receptors). It is known that Xeplion has a low affinity for histamine receptors and therefore the sedative effect is practically absent. In turn, rispolept-consta, on the contrary, has a higher affinity for histamine receptors, which causes a moderate sedative effect and an effect on affective symptoms. Xeplion has a positive effect on sleep disorders, so it is more acceptable in patients with depressive symptoms (an antidepressant effect has been described). In our clinical practice, we actually noted that Xeplion has a more pronounced antidepressant effect, while Rispolept-Consta may be preferable for manic symptoms.

Today, in most cases, the choice of a drug for maintenance therapy is determined by its effectiveness and ease of use both for the doctor and, of course, first of all, for the patient himself. Therefore, when choosing a drug, we give preference to Xeplion. In cases where the frequency of injections is not critical for the patient and the clinical picture allows, rispolept-consta is prescribed. Of course, it is necessary to take into account the economic component and storage capabilities (rispolept-consta requires low-temperature storage, as well as certain cooking conditions). In addition, when prescribing Rispolept-Consta or Xeplion, we take into account the patient’s adherence to a particular therapy, our real economic capabilities and the availability of the drug in pharmacies.

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Contraindications

• the patient has hypersensitivity to the components of the drug;
• glaucoma (especially angle-closure );
• atrial fibrillation , tachyarrhythmia ;
• prostate adenoma;
• intestinal atony and atonic constipation ;
• megacolon , intestinal obstruction ;
• gastrointestinal obstruction;
• pregnancy, lactation.

Use with caution

Patients with cardiovascular diseases, liver or kidney disorders.

Side effects of Cyclodol

• skin rash;
• dry mouth;
• drowsiness;
• nervousness;
• dizziness;
• impaired visual acuity;
• development of increased intraocular pressure, therefore regular checks are recommended during therapy;
• urinary retention, constipation;
• tachycardia;
• delirium and hallucinations are possible .

Side effects of Cyclodol with long-term use can be expressed in the form of purulent mumps.

Cyclodol, instructions for use (Method and dosage)

The tablets should be taken orally during or before meals.

The dosage should be selected individually - even a slight overdose of the drug causes an “intoxicating effect” and hallucinations . Therefore, the patient can experience a so-called trip - a psychedelic state, an altered consciousness that differs from typical perception and awareness (source - Wikipedia). Therefore, patients should know what it is and consult their doctor in time, since the tolerability of the drug varies significantly among different patients.

Typically, the initial daily dose is 0.5-1 mg (divided into 3-4 doses); in order to achieve optimal effect, it can subsequently be increased by 1-2 mg every 3-5 days. The maximum single dose for adults is no more than 10 mg, per day - up to 16 mg.

Attention!

Therapy should be discontinued gradually over 1-2 weeks, as there is a risk of exacerbation of symptoms of parkinsonism , a potentially fatal neuroleptic malignant syndrome accompanied by hyperpyrexia , muscle rigidity , changes in mental status, and autonomic dysfunction. Patients should be advised of the risk of developing addiction (especially if they have mental illness).

The duration of treatment is determined by the doctor separately for each case.

Special patient groups

Patients over 60 years of age are recommended to take half the standard dose, as the risk of adverse reactions and hypersensitivity is increased.

Instructions for use of Cyclodol with Levodopa

The daily dose of Cyclodol should not exceed 3–6 mg.

Cyclodol 2 mg No. 50 tablet.

Instructions for use of the medicinal product for consumers (insert leaflet) CYCLODOL GRINDEX Before using the medicinal product, be sure to consult a doctor and carefully read the instructions! Trade name Cyclodol Grindeks International nonproprietary name Trihexyphenidyl Dosage form Tablets 2 mg Composition One tablet contains the active substance - trihexyphenidyl hydrochloride 2 mg. excipients: sucrose, potato starch, microcrystalline cellulose, calcium stearate. Description Round flat-cylindrical tablets of white color with a chamfer. Pharmacological properties Pharmacokinetics When administered orally, trihexyphenidyl is quickly and completely absorbed from the digestive tract. The effect is achieved within an hour. The half-life is 5-10 hours. Trihexyphenidyl is highly lipotropic and passes well through the blood-brain and placental barriers. Trihexyphenidyl is hydrolyzed in tissues under the action of nonspecific esterases on alcohol and organic acids; a small part of trihexyphenidyl is excreted unchanged through the kidneys. Pharmacodynamics Cyclodol Grindeks is a synthetic anticholinergic blocker that reduces tremor, muscle rigidity and bradykinesia characteristic of parkinsonism. Cyclodol Grindeks has a strong m-anticholinergic and weak n-anticholinergic effect. The mechanism of action is based on its ability to compete with acetylcholine on the postsynaptic membrane. Indications for use - parkinsonism - extrapyramidal disorders caused by drugs. Method of administration and dosage. The dosage is selected individually. The drug should be taken before meals. Start taking it with a dosage of 1 mg per day. The dose is increased gradually by 2 mg every 3-5 days. The usual maintenance dose is 6-10 mg per day, divided into 3-4 doses. In severe cases, it may be necessary to increase the dose to 12-16 mg, divided into 3-4 doses. The maximum daily dose is 16 mg trihexyphenidyl. The duration of treatment is prescribed individually. Upon completion of treatment or if alternative treatment is initiated, the dose of trihexyphenidyl should be reduced gradually. Elderly patients are more sensitive to this drug and should use lower doses. Not used in pediatric practice. Side effects Often: - mydriasis, accommodation disturbances, photophobia - dry mouth, decreased sweating, constipation - stomach pain, nausea. Uncommon: - urinary retention - tachycardia (very rarely - bradycardia) - increased sensitivity Rare: - angle-closure glaucoma, which is associated with increased intraocular pressure, so it is necessary to regularly monitor intraocular pressure. - fatigue, drowsiness, dizziness, nervousness, insomnia, memory impairment Very rarely - bradycardia When using large doses or when treating patients with predisposing factors (atherosclerosis, advanced age or patients with idiosyncrasy to any drug), the following may occur: - clouding of consciousness and other mental disorders - unnatural increase in mood, agitation, irritation - vomiting or nausea. In this case, it is necessary to stop treatment. When the dosage is reduced or treatment is stopped, the side effects disappear. Contraindications - hypersensitivity to trihexyphenidyl and/or excipients - untreated urinary retention - benign prostatic hypertrophy with urinary retention - closed-angle glaucoma - digestive tract obstruction - tachyarrhythmias - acute intoxication with alcohol, psychotropic drugs or opiates - acute delirium and mania - tardive dyskinesia (tardive dyskinesia) - pathological movements - a side effect of long-term use of antipsychotic drugs. Drug interactions The effect of trihexyphenidyl may be enhanced when used together with other anticholinergic drugs with similar properties (for example, amantadine, some histamine blockers, phenothiazine derivatives, tricyclic antidepressants, etc.) and together with MAO inhibitors (they inhibit enzymes that metabolize drugs). When used together with these medications, the following side effects may occur: dry mouth, blurred vision, urinary retention and constipation. Trihexyphenidyl and parasympathomimetics act antagonistically. With simultaneous use of trihexyphenidyl, the effect of sublingually applied nitrates is reduced (due to dry mouth). Inhibition of intestinal motility by trihexyphenidyl may interfere with the absorption of other drugs. Trihexyphenidyl reduces the effects of metoclopramide and domperidone on the digestive tract. The depressive effects of alcohol and other drugs may be enhanced when used with trihexyphenidyl. When used together with levodopa, the dosage of both drugs must be reduced. Usually in this case, 3-6 mg of trihexyphenidyl per day, divided into two doses, is sufficient. Special instructions Trihexyphenidyl should be used very carefully in elderly patients and in patients with cardiovascular diseases, impaired liver and kidney function. Caution is necessary in the following cases: diseases that can lead to life-threatening tachycardia, dementia syndrome, myasthenia gravis, prostatic hypertrophy with complete emptying of the bladder. There are known cases of abuse of trihexyphenidyl, especially in psychiatric patients (due to hallucinating and euphoric effects). It should be taken into account that drug dependence may develop. Treatment should not be stopped suddenly. Pregnancy and lactation The drug passes through the placental barrier and is excreted in breast milk, as a result of which it is undesirable to use the drug during pregnancy and lactation. Features of the effect of the drug on the ability to drive vehicles or potentially dangerous mechanisms. Caution should be exercised because the drug affects the reaction rate. Overdose Symptoms: Large doses of trihexyphenidyl cause blockade of the postganglionic endings of the parasympathetic nervous system, the picture of poisoning corresponds, in principle, to atropine poisoning (mydriasis, dry mucous membranes, tachycardia, atony of the intestines and biliary tract, elevated body temperature, etc.). Trihexyphenidyl also causes disorders of the central nervous system (irritability, disturbances of consciousness, derealization and other mental disorders). With more severe poisoning, coma or paralysis of the respiratory center may occur. Treatment: There is no specific antidote. It is necessary to perform gastric lavage and use other possible methods to reduce the absorption of the drug. Treatment is symptomatic: cold compresses, drinking plenty of fluids. Cholinesterase inhibitors (eg, physostigmine) can be used; sodium bicarbonate or sodium lactate have been used successfully to treat cardiac complications, diazepam for seizures, and physostigmine for delirium. Release form and packaging 2 mg tablets, 25 tablets in a blister, 2 blisters in a cardboard pack along with instructions for use. Storage conditions Store in a place protected from light at a temperature not exceeding 25°C. Keep out of the reach of children! Shelf life: 5 years. Do not use after the expiration date stated on the package. Conditions for dispensing from pharmacies By prescription Manufacturer JSC GRINDEX. St. Krustpils 53, Riga, LV-1057, Latvia.

Overdose

Clinical picture

Facial hyperemia, dry skin and mucous membranes, difficulty swallowing, elevated temperature, dilated pupils, muscle weakness, impaired urination, decreased intestinal motility, tachycardia , heart rhythm disturbances, neuropsychiatric disorders, including delirium , disorientation , anxiety, agitation, aggressiveness, hallucinations , incoherence , confusion, ataxia , paranoid reactions , convulsions . The patient's condition may worsen to central depression , coma and even death .

Treatment

Since an overdose of trihexyphenidyl can lead to dangerous poisoning, immediate first aid is necessary:

• hemodialysis or hemoperfusion (only in the first hours after poisoning);
• the use of bicarbonate or sodium lactate helps eliminate complications from the cardiovascular system;
• physostigmine (administered by infusion 2-8 mg for 20-40 minutes to counteract - Atropine ) is effective for the treatment of such symptoms of intoxication as: delirium , coma , extrapyramidal disorders , tachyarrhythmia , frequent ventricular extrasystoles, various blockades.

Analogs

Level 4 ATX code matches:
Parkopan

Akineton

Structural analogues (active substance – Trihexyphenidyl ):

• Parkopan;
• Tryphen.

When Cyclodol therapy leads to serious side effects, causes addiction, or the body simply becomes resistant to the drug, patients ask about the possibility of replacing Cyclodol.

Akineton or Cyclodol - which is better?

Akineton is also a central anticholinergic blocker with an active substance - biperiden , available both in the form of tablets and solution for injection. It is considered somewhat better, as it has a smaller list of side effects and affects cognitive functions to a lesser extent.

Overdose with cyclodol

articles » Drug addiction » Overdose with cyclodol
Overdose with cyclodol rarely leads to death. However, this does not mean at all that you can use it as much as you want. Let's start with the fact that you shouldn't use drugs at all, no matter how strong the effect they have. Any drug is addictive and ultimately leads to irreversible changes in the body, which ultimately end in death...

Let's start with the fact that cyclodol is a medical drug that began to be used in domestic medicine in the middle of the last century. At that time, this drug was almost the only one that helped people suffering from parkinsonism. Very soon after the start of its use in medicine, doctors discovered that an overdose of cyclodol (even the most minimal) leads to an intoxicating effect. If you take too much of this drug, the person may experience hallucinations. Soon this drug went beyond the hospital walls and began to be used among drug addicts. Why not? After all, it causes euphoria, and even provokes hallucinations!

Roughly speaking, an overdose of cyclodol is what every drug addict does when he uses this substance. Medical doses of this drug do not lead to an intoxicating effect and certainly do not provoke hallucinations. This is why drug addicts use this substance in large quantities. However, they still have a measure. After all, if they use this medicine in too large quantities, then their vital organs may even fail.

An overdose of cyclodol causes effects that can be divided into the following phases:

First phase

The person’s mood rises and he plunges into a state of euphoria. Usually this condition occurs 20 minutes after taking the tablets. Externally, the first phase manifests itself in loquaciousness, constant laughter and increased mobility. A person at this stage seems to be deprived of any problems.

Second phase

The first phase lasts no more than twenty minutes and then gives way to the second - far from the most pleasant. The person experiences retardation in movement. He no longer wants to have fun, but only one desire appears - to lie down on the bed. This stage of cyclodol overdose is notable for the fact that the person becomes suggestible. While exploring this issue, in the work of one scientist working on this drug, we found an example from his experience in which he said that once a girl under the influence of cyclodol was raped by eleven people. Just imagine how much you need to lose control over yourself to allow this to happen!

A significant overdose of cyclodol also provokes the third and fourth phases. The third phase is characterized by the appearance of hallucinations and loss of orientation in time and space. In the fourth phase, the person “let go”: his body becomes heavy and exhausted. As a rule, this phase ends with a long restorative sleep.

Reviews about Cyclodol

There are many opinions, discussions and topics on forums about the advisability of using Cyclodol. It is used for therapeutic purposes - for Parkinson's disease , schizophrenia , etc., and also as an antidepressant or to achieve a state of altered consciousness - the so-called “cyclodol addicts”.

Reviews of Cyclodol agree on one thing - the drug has a strong impact on vision, the urinary system, cognitive functions, causes addiction and severe withdrawal syndrome ( choline rebound ). However, there are examples when the dosage of the drug is selected correctly and patients use the medicine for decades.

It all depends on individual susceptibility, the nature and severity of the disease, and, of course, the professionalism of the attending physician.